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Beconase-AQ

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Beconase-AQ

CLINICAL PHARMACOLOGY

Mechanism of Action

Following topical administration, beclomethasone dipropionate produces anti-inflammatory and vasoconstrictor effects. The mechanisms responsible for the anti-inflammatory action of beclomethasone dipropionate are unknown. Corticosteroids have been shown to have a wide range of effects on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, and cytokines) involved in inflammation. The direct relationship of these findings to the effects of beclomethasone dipropionate on allergic rhinitis symptoms is not known.

Biopsies of nasal mucosa obtained during clinical studies showed no histopathologic changes when beclomethasone dipropionate was administered intranasally.

Beclomethasone dipropionate is a pro-drug with weak glucocorticoid receptor binding affinity. It is hydrolyzed via esterase enzymes to its active metabolite beclomethasone-17-monopropionate (B-17-MP), which has high topical anti-inflammatory activity.

Pharmacokinetics

Absorption: Beclomethasone dipropionate is sparingly soluble in water. When given by nasal inhalation in the form of an aqueous or aerosolized suspension, the drug is deposited primarily in the nasal passages. The majority of the drug is eventually swallowed. Following intranasal administration of aqueous beclomethasone dipropionate, the systemic absorption was assessed by measuring the plasma concentrations of its active metabolite B-17-MP, for which the absolute bioavailability following intranasal administration is 44% (43% of the administered dose came from the swallowed portion and only 1% of the total dose was bioavailable from the nose). The absorption of unchanged beclomethasone dipropionate following oral and intranasal dosing was undetectable (plasma concentrations < 50 pg/mL).

Distribution: The tissue distribution at steady state for beclomethasone dipropionate is moderate (20 L) but more extensive for B-17-MP (424 L). There is no evidence of tissue storage of beclomethasone dipropionate or its metabolites. Plasma protein binding is moderately high (87%).

Metabolism: Beclomethasone dipropionate is cleared very rapidly from the systemic circulation by metabolism mediated via esterase enzymes that are found in most tissues. The main product of metabolism is the active metabolite (B-17-MP). Minor inactive metabolites, beclomethasone-21-monopropionate (B-21-MP) and beclomethasone (BOH), are also formed, but these contribute little to systemic exposure.

Elimination: The elimination of beclomethasone dipropionate and B-17-MP after intravenous administration are characterized by high plasma clearance (150 and 120 L/hour) with corresponding terminal elimination half-lives of 0.5 and 2.7 hours. Following oral administration of tritiated beclomethasone dipropionate, approximately 60% of the dose was excreted in the feces within 96 hours, mainly as free and conjugated polar metabolites. Approximately 12% of the dose was excreted as free and conjugated polar metabolites in the urine. The renal clearance of beclomethasone dipropionate and its metabolites is negligible.

Pharmacodynamics: The effects of beclomethasone dipropionate on hypothalamic-pituitary-adrenal (HPA) function have been evaluated in adult volunteers by other routes of administration. Studies with beclomethasone dipropionate by the intranasal route may demonstrate that there is more or that there is less absorption by this route of administration. There was no suppression of early morning plasma cortisol concentrations when beclomethasone dipropionate was administered in a dose of 1,000 mcg/day for 1 month as an oral aerosol or for 3 days by intramuscular injection. However, partial suppression of plasma cortisol concentrations was observed when beclomethasone dipropionate was administered in doses of 2,000 mcg/day either by oral aerosol or intramuscular injection. Immediate suppression of plasma cortisol concentrations was observed after single doses of 4,000 mcg of beclomethasone dipropionate. Suppression of HPA function (reduction of early morning plasma cortisol levels) has been reported in adult patients who received 1,600-mcg daily doses of oral beclomethasone dipropionate for 1 month. In clinical studies using beclomethasone dipropionate aerosol intranasally, there was no evidence of adrenal insufficiency. The effect of BECONASE AQ Nasal Spray on HPA function was not evaluated but would not be expected to differ from intranasal beclomethasone dipropionate aerosol.

In 1 study in children with asthma, the administration of inhaled beclomethasone at recommended daily doses for at least 1 year was associated with a reduction in nocturnal cortisol secretion. The clinical significance of this finding is not clear. It reinforces other evidence, however, that topical beclomethasone may be absorbed in amounts that can have systemic effects and that physicians should be alert for evidence of systemic effects, especially in chronically treated patients (see PRECAUTIONS).

Last reviewed on RxList: 6/20/2008
This monograph has been modified to include the generic and brand name in many instances.

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